Related Experiment Video

Updated: May 16, 2025

Methods for Evaluating the Role of c-Fos and Dusp1 in Oncogene Dependence
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Published on: January 7, 2019

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Rethinking MYC inhibition: a multi-dimensional approach to overcome cancer's master regulator

Jing Yu1, Dan Liu1, Yujian Yuan2

  • 1Qingdao Hospital, University of Health and Rehabilitation Sciences, Qingdao, Municipal Hospital, Qingdao, China.

Frontiers in Cell and Developmental Biology
|May 14, 2025
PubMed

Insights

MYC oncoprotein, once considered undruggable, is now targeted by novel inhibitors and degraders, offering new hope for MYC-driven cancers. Combination therapies and biomarker-guided strategies are key to overcoming challenges and improving patient outcomes.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • The MYC oncoprotein is a critical regulator in cancer development.
  • MYC's disordered structure historically made it a challenging therapeutic target.
  • Recent breakthroughs are enabling direct targeting of MYC.

Purpose of the Study:

  • To review recent advances in targeting the MYC oncoprotein.
  • To discuss emerging therapeutic strategies and their clinical potential.
  • To advocate for a comprehensive approach to MYC-targeted cancer therapy.

Main Methods:

  • Review of direct MYC inhibitors (e.g., Omomyc).
  • Analysis of PROTAC-based MYC degraders (e.g., WBC100).
  • Exploration of complementary strategies including BET/CDK9 inhibitors, RNA therapeutics, nanobodies, and engineered proteases.

Main Results:

  • Direct MYC inhibitors and PROTAC degraders show promising clinical progress.
  • Diverse therapeutic modalities are expanding the landscape of MYC targeting.
  • Combination therapies with chemotherapy, radiotherapy, or immunotherapy exhibit synergistic effects.

Conclusions:

  • MYC is emerging as a druggable target in oncology.
  • Challenges in specificity, toxicity, and delivery persist but are being addressed.
  • A multi-dimensional, biomarker-guided approach with rational drug combinations is crucial for effective MYC-driven cancer treatment.
Keywords:
MYC inhibitioncancer therapycombination therapiesdirect MYC targetingindirect MYC targeting

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